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Raising High-Density Lipoprotein in Humans Through Inhibition of Cholesteryl Ester Transfer Protein: An Initial Multidose Study of Torcetrapib
TLDR
These effects of CETP inhibition resemble those observed in partial CETP deficiency, and serve as a prelude to further studies in subjects with low HDL, or combinations of dyslipidemia, in assessing the role of CETp in atherosclerosis. Expand
Cell Toxicity Induced by Inhibition of Acyl Coenzyme A:Cholesterol Acyltransferase and Accumulation of Unesterified Cholesterol *
TLDR
Results suggest that ACAT inhibition of cholesterol-enriched macrophages increases cell toxicity due to the buildup of cellular free cholesterol, and removal of free cholesterol by the addition of extracellular cholesterol acceptors or by blocking intracellular sterol transport relieves the ACAT inhibitor-induced toxicity. Expand
Description of the torcetrapib series of cholesteryl ester transfer protein inhibitors, including mechanism of actions⃞
TLDR
It is demonstrated that a series of potent cholesteryl ester transfer protein (CETP) inhibitors bind specifically to CETP with 1:1 stoichiometry and block both neutral lipid and phospholipid transfer activities. Expand
Post-translational changes in tertiary and quaternary structure of the insulin proreceptor. Correlation with acquisition of function.
TLDR
Tertiary and quaternary structural changes that occur during post-translational processing of the insulin proreceptor were examined in 3T3-L1 adipocytes, revealing that the M2 species acquires insulin binding activity and an epitope recognized by a binding site specific autoimmune antibody through a subtle structural change not detected by reducing or nonreducing SDS-polyacrylamide gel electrophoresis. Expand
Polymorphisms in the CETP gene and association with CETP mass and HDL levels.
TLDR
The coding regions, adjacent introns, and proximal 5' and 3' regions were resequenced from an ethnically diverse population and novel and previously known polymorphisms were characterized and associations with HDL and CETP mass levels determined. Expand
Mechanism of the hepatic lipase induced accumulation of high-density lipoprotein cholesterol by cells in culture.
TLDR
Experiments utilizing HDL reconstituted with 14C-free cholesterol and [3H]cholesteryl oleoyl ether suggest that hepatic lipase enhances the incorporation of HDL-esterified cholesterol, which was 4-fold that of esterified cholesterol. Expand
Inhibition of Cholesteryl Ester Transfer Protein by Torcetrapib Modestly Increases Macrophage Cholesterol Efflux to HDL
TLDR
Data indicate that inhibition of CETP by torcetrapib causes a modest increase in the ability of HDL to promote net cholesterol efflux at the 60 mg dose, and a more dramatic increase at the 120 mg dose in association with enhanced particle functionality. Expand
The bidirectional flux of cholesterol between cells and lipoproteins. Effects of phospholipid depletion of high density lipoprotein.
TLDR
In the presence of an inhibitor of acyl coenzyme A:cholesterol acyltransferase, the steady state distribution of FC mass between cells and HDL was accurately predicted by the ratio of rate constants for FC flux, providing additional validation for describing FC flux in terms of first-order rate constants and homogeneous cell and HDL FC pools. Expand
Hepatic lipase stimulates the uptake of high density lipoprotein cholesterol by hepatoma cells.
TLDR
The enhanced cellular accumulation of HDL free cholesterol observed with hepatic lipase appears to be due to the phospholipase activity of this enzyme, since similar results were obtained with HDL that had been modified by snake venom phospholIPase A2. Expand
Reverse cholesterol transport.
TLDR
This chapter focuses on the process of reverse cholesterol transport, whereby cholesterol molecules enter the “reverse cholesterol transport” pathway whereby they are delivered to the liver, converted to bile acids, and then excreted from the body. Expand
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